PROTAC AR-NTD degrader 1

• UNSPSC Description:

  PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively[1].

• Target Antigen:

  Androgen Receptor; Apoptosis

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Vitamin D Related/Nuclear Receptor

• Applications:

  Cancer-programmed cell death

• Field of Research:

  cancer

• Assay Protocol:

  https://www.medchemexpress.com/protac-ar-ntd-degrader-1.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(N1)CCC(N2C(C3=CC=C(C=C3C2=O)NCCCN4N=NC(CCCCCOC5=CC=C(C(C)(C)C6=CC=C(OC[C@@H](CCl)O)C=C6)C=C5)=C4)=O)C1=O

• Molecular Weight:

  771.30

• References & Citations:

  [1]Zhang B, et al. Discovery of BWA-522, a First-in-Class and Orally Bioavailable PROTAC Degrader of the Androgen Receptor Targeting N-Terminal Domain for the Treatment of Prostate Cancer. J Med Chem. 2023 Aug 24;66(16):11158-11186..

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  3032601-92-3